Quaternary salts of 4,3' and 4,4' bis-pyridinium monooximes: synthesis and biological activity
| Autor: | Garlapati Achaiah, Chennamaneni Srinivas Rao, Vobalaboina Venkateswarlu |
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| Rok vydání: | 2005 |
| Předmět: |
Cholinesterase Reactivators
Pyridinium Compounds medicine.drug_class Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Chloride Medicinal chemistry Chemical synthesis chemistry.chemical_compound Mice Structure-Activity Relationship Drug Discovery Oximes medicine Organic chemistry Animals Molecular Biology Organic Chemistry Brain Oxime Enzyme Activation chemistry Tetraethyl pyrophosphate Acetylcholinesterase Molecular Medicine Pyridinium Cholinesterase Inhibitors medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry letters. 15(12) |
| ISSN: | 0960-894X |
| Popis: | Six unsymmetrical bis-quaternary monooximes viz. dibromides of 1-(4-hydroxyiminomethyl pyridinium)-3-(3/4-carbamoyl pyridinium)propane, 1-(4-hydroxyiminomethyl pyridinium)-4-(3/4-carbamoyl pyridinium) butane, 1-(4-hydroxyiminomethyl pyridinium)-5-(3/4-carbamoyl pyridinium)pentane were synthesized and characterized by spectral data. Their ability to reactivate tetraethyl pyrophosphate inhibited mouse total brain cholinesterase was investigated and compared with 2-pyridine aldoxime chloride (2-PAM). All the compounds were found to be more effective acetylcholinesterase reactivators when compared with the conventional oxime, 2-PAM, except the compound (5a) with pentylene bridge and carbamoyl group present at fourth position. The bis-pyridinium monooximes with 3-carbamoyl group were more potent reactivators than the corresponding 4-carbamoyl compounds and bis-oximes tested. |
| Databáze: | OpenAIRE |
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